Gabapentin

Gabapentin
Chemical Nomenclature
Common names	Gabapentin, Neurontin, Gabarone, Gralise
Substitutive name	Gabapentin
Systematic name	1-(Aminomethyl)cyclohexaneacetic acid
Class Membership
Psychoactive class	Depressant
Chemical class	Gabapentinoid
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Oral Dosage Bioavailability 27% - 60% Threshold 200 mg Light 200 - 900 mg Common 900 - 1500 mg Strong 1500 - 2400 mg Heavy 2400 mg + Duration Total 6 - 10 hours Onset 30 - 120 minutes Peak 120 - 180 minutes DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Interactions
Opioids
Depressants

Gabapentin, marketed under the brand name Neurontin among others, is a medication used as an anticonvulsant and analgesic. Originally it was developed to treat epilepsy, and is currently used to relieve neuropathic pain and restless leg syndrome.[3] It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.[4]

Gabapentin is also an effective tool for treating social anxiety disorder, panic disorder[20][21] and generalized anxiety disorder.[6][7]

It is a structural analogue of the inhibitory neurotransmitter γ-aminobutyric acid (GABA).

Chemistry

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Pharmacology

Gabapentin was initially synthesized to mimic the chemical structure of the neurotransmitter gamma-aminobutyric acid (GABA), but is believed to act on different brain receptors.[citation needed]

Some of its activity may involve interaction with voltage-gated calcium channels. Gabapentin binds to the α2δ subunit (1 and 2) and has been found to reduce calcium currents after chronic but not acute application via an effect on trafficking[47] of voltage-dependent calcium channels in the central nervous system.[48] Another possible mechanism of action is that gabapentin halts the formation of new synapses.[49]

Subjective effects

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Toxicity and harm potential

The most common side effects of gabapentin in adult patients include dizziness, fatigue, drowsiness, weight gain, and peripheral edema (swelling of extremities).[39] Gabapentin may also produce sexual dysfunction in some patients, symptoms of which may include loss of libido, inability to reach orgasm, and erectile dysfunction.[40][41] Gabapentin should be used carefully in patients with renal impairment due to possible accumulation and toxicity.[42]

An increase in formation of adenocarcinomas was observed in rats during preclinical trials; however, the clinical significance of these results remains undetermined. Gabapentin is also known to induce pancreatic acinar cell carcinomas in rats through an unknown mechanism, perhaps by stimulation of DNA synthesis; these tumors did not affect the lifespan of the rats and did not metastasize.[43]

Suicide

In 2009 the U.S. Food and Drug Administration issued a warning of an increased risk of depression and suicidal thoughts and behaviors in patients taking gabapentin, along with other anticonvulsant drugs[44] modifying the packaging insert to reflect this.[39] A 2010 meta analysis confirmed the increased risk of suicide associated with gabapentin use.[45]

Lethal dosage

Persons who accidentally or intentionally ingested overdoses may have drowsiness, sedation, blurred vision, slurred speech, somnolence and possibly death, if a very high amount was taken, particularly if combined with alcohol. Serum gabapentin concentrations may be measured to confirm diagnosis.[46]

References

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